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WO2004056779A3 - Derives de tetrahydroquinoline - Google Patents

Derives de tetrahydroquinoline Download PDF

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Publication number
WO2004056779A3
WO2004056779A3 PCT/EP2003/051024 EP0351024W WO2004056779A3 WO 2004056779 A3 WO2004056779 A3 WO 2004056779A3 EP 0351024 W EP0351024 W EP 0351024W WO 2004056779 A3 WO2004056779 A3 WO 2004056779A3
Authority
WO
WIPO (PCT)
Prior art keywords
alkyl
amino
alkylamino
derivatives
receptor modulators
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/EP2003/051024
Other languages
English (en)
Other versions
WO2004056779A2 (fr
Inventor
Cornelis Marius Timmers
Willem Frederik Johan Karstens
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Akzo Nobel NV
Original Assignee
Akzo Nobel NV
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to EP03808299A priority Critical patent/EP1578727B1/fr
Priority to HK05112053.4A priority patent/HK1077576B/en
Priority to MXPA05006772A priority patent/MXPA05006772A/es
Priority to AU2003303221A priority patent/AU2003303221B2/en
Priority to NZ540577A priority patent/NZ540577A/en
Priority to CA2508923A priority patent/CA2508923C/fr
Priority to SI200331217T priority patent/SI1578727T1/sl
Priority to BR0317514-6A priority patent/BR0317514A/pt
Priority to HR20050577A priority patent/HRP20050577A2/hr
Priority to JP2004561498A priority patent/JP4545000B2/ja
Priority to DE60320457T priority patent/DE60320457T2/de
Application filed by Akzo Nobel NV filed Critical Akzo Nobel NV
Priority to YUP-2005/0458A priority patent/RS51196B/sr
Priority to UAA200505286A priority patent/UA80303C2/uk
Priority to US10/540,335 priority patent/US7674909B2/en
Priority to ES03808299T priority patent/ES2304544T3/es
Priority to DK03808299T priority patent/DK1578727T3/da
Publication of WO2004056779A2 publication Critical patent/WO2004056779A2/fr
Publication of WO2004056779A3 publication Critical patent/WO2004056779A3/fr
Priority to IS7870A priority patent/IS2553B/is
Priority to NO20052777A priority patent/NO330640B1/no
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/38—Nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18—Feminine contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
    • A61P5/08—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH for decreasing, blocking or antagonising the activity of the anterior pituitary hormones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La présente invention porte sur des dérivés de tétrahydroquinoline de formule générale (I) ou sur un sel de ceux-ci acceptable d'un point de vue pharmaceutique. Dans cette formule, R1 et R2 représentent H, Me; R3 représente (2-6C)hétérocycloalkyl(1--4C)alkyle, (2-5C)hétéroaryl(1-4C)alkyle, (6C)aryle (1-4C)alkyle, (1-4C)(di)alkylaminocarbonylamino(2-4C)alkyle, (2--6C) hétérocycloalkylcarbonylamino(2-4C)alkyle, R5-(2-4C)alkyle ou R5-carbonyl(1-4C)alkyle; R4 représente (2-5C)hétéroaryle, (6C)aryle, (3-8C)cycloalkyle, (2-6C)hétérocycloalkyle ou (1-6C) alkyle et R5 représente (di)(1-4C)alkylamino, (1-4C)alcoxy, amino, hydroxy, (6C)arylamino, (di)(3-4C)alcénylamino, (2-5C)hétéroaryl(1-4C)alkylamino, (6C)aryl(1-4C) alkylamino, (di)[(1--4C)alcoxy(2-4C)alkyl]amino, (di)[(1-4C)alkylamino(2-4C) alkyl]amino, (di)[amino(2-4C)alkyl]amino ou (di)[hydroxy(2--4C)alkyl]amino. La présente invention porte également sur des compositions pharmaceutiques comprenant ces dérivés et sur leur utilisation afin de réguler la fécondité.
PCT/EP2003/051024 2002-12-20 2003-12-16 Derives de tetrahydroquinoline Ceased WO2004056779A2 (fr)

Priority Applications (18)

Application Number Priority Date Filing Date Title
DE60320457T DE60320457T2 (de) 2002-12-20 2003-12-16 Tetrahydrochinolin-derivate und deren verwendung als modulatoren des fsh-rezeptors
MXPA05006772A MXPA05006772A (es) 2002-12-20 2003-12-16 Derivados de tetrahidroquinolina.
AU2003303221A AU2003303221B2 (en) 2002-12-20 2003-12-16 Tetrahydroquinoline derivatives and their use as FSH receptor modulators
NZ540577A NZ540577A (en) 2002-12-20 2003-12-16 Tetrahydroquinoline derivatives and their use as FSH receptor modulators
CA2508923A CA2508923C (fr) 2002-12-20 2003-12-16 Derives de tetrahydoquinoline et leur utilisation en tant modultateurs du recepteur fsh
SI200331217T SI1578727T1 (sl) 2002-12-20 2003-12-16 Tetrahidrokinolinski derivati in njihova uporaba kot modulatorji receptorja FSH
YUP-2005/0458A RS51196B (sr) 2002-12-20 2003-12-16 Derivati tetrahidrohinolina
HK05112053.4A HK1077576B (en) 2002-12-20 2003-12-16 Tetrahydroquinoline derivatives and their use as fsh receptor modulators
JP2004561498A JP4545000B2 (ja) 2002-12-20 2003-12-16 テトラヒドロキノリン誘導体及びｆｓｈ受容体モジュレーターとしてのその使用
EP03808299A EP1578727B1 (fr) 2002-12-20 2003-12-16 Derives de tetrahydroquinoleine et leurs utilisations en tant que modulateurs durecepteur de fsh
HR20050577A HRP20050577A2 (en) 2002-12-20 2003-12-16 Tetrahydroquinoline derivatives
BR0317514-6A BR0317514A (pt) 2002-12-20 2003-12-16 Derivado de tetraidroquinolina, composição farmacêutica, e, uso do derivado de tetraidroquinolina
UAA200505286A UA80303C2 (en) 2002-12-20 2003-12-16 Tetrahydroquinoline derivatives, pharmaceutical composition based thereon and their use
US10/540,335 US7674909B2 (en) 2002-12-20 2003-12-16 Tetrahydroquinoline derivatives and their use as FSH receptor modulators
ES03808299T ES2304544T3 (es) 2002-12-20 2003-12-16 Derivados de tetrahidroquinoleina y sus utilizaciones como moduladores del receptor de fsh.
DK03808299T DK1578727T3 (da) 2002-12-20 2003-12-16 Tetrahydroquinolin-derivater og deres anvendelse som FSH-receptor-modulatorer
IS7870A IS2553B (is) 2002-12-20 2005-05-26 Tetrahýdrókínólín afleiður og notkun þeirra sem FSH viðtakastillar.
NO20052777A NO330640B1 (no) 2002-12-20 2005-06-08 Tetrahydrokinolinderivater, farmasoytiske preparater omfattende slike, slike forbindelser for anvendelse i terapi samt anvendelse av slike for fremstilling av medikament for fruktbarhetskontroll

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US43547902P 2002-12-20 2002-12-20
EP02102865 2002-12-20
EP02102865.9 2002-12-20
US60/435,479 2002-12-20

Publications (2)

Publication Number Publication Date
WO2004056779A2 WO2004056779A2 (fr) 2004-07-08
WO2004056779A3 true WO2004056779A3 (fr) 2004-08-12

Family

ID=38799446

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2003/051024 Ceased WO2004056779A2 (fr) 2002-12-20 2003-12-16 Derives de tetrahydroquinoline

Country Status (23)

Country Link
US (1) US7674909B2 (fr)
EP (1) EP1578727B1 (fr)
JP (1) JP4545000B2 (fr)
AR (1) AR042629A1 (fr)
AT (1) ATE392416T1 (fr)
AU (1) AU2003303221B2 (fr)
BR (1) BR0317514A (fr)
CA (1) CA2508923C (fr)
CL (1) CL43546B (fr)
DE (1) DE60320457T2 (fr)
DK (1) DK1578727T3 (fr)
ES (1) ES2304544T3 (fr)
MX (1) MXPA05006772A (fr)
NZ (1) NZ540577A (fr)
PE (1) PE20040799A1 (fr)
PL (1) PL376997A1 (fr)
PT (1) PT1578727E (fr)
RS (1) RS51196B (fr)
RU (1) RU2328487C2 (fr)
SI (1) SI1578727T1 (fr)
TW (1) TWI322012B (fr)
UA (1) UA80303C2 (fr)
WO (1) WO2004056779A2 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9174940B2 (en) 2007-08-31 2015-11-03 Merck Sharp & Dohme B.V. TSH receptor antagonizing tetrahydroquinoline compounds

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL159288A0 (en) * 2001-07-02 2004-06-01 Akzo Nobel Nv Tetrahydroquinoline derivatives
TWI306855B (en) * 2002-12-20 2009-03-01 Organon Nv Tetrahydroquinoline derivatives
DE10260739B3 (de) 2002-12-23 2004-09-16 Outokumpu Oy Verfahren und Anlage zur Herstellung von Metalloxid aus Metallverbindungen
US7691848B2 (en) 2005-03-02 2010-04-06 Wyeth Pyrrolobenzodiazepine arylcarboxamides and derivatives thereof as follicle-stimulating hormone receptor antagonists
UA92007C2 (ru) * 2005-05-04 2010-09-27 Н.В. Органон Производные 4-фенил-5-оксо-1,4,5,6,7,8-гексагидрохинолина для лечения бесплодности
UA92008C2 (en) * 2005-05-04 2010-09-27 Н.В. Органон 4-PHENYL-5-OXO-l,4,5,6,7,8-HEXAHYDROQUINOLINE DERIVATIVES AS MEDICAMENTS FOR THE TREATMENT OF INFERTILITY
JP4869336B2 (ja) 2005-05-04 2012-02-08 ナームローゼ・フエンノートチヤツプ・オルガノン ジヒドロピリジン誘導体
UA92009C2 (ru) * 2005-05-04 2010-09-27 Н.В. Органон Производные 4-фенил-5-оксо-1,4,5,6,7,8-гексагидрохинолина для лечения бесплодия
JP2008540567A (ja) 2005-05-12 2008-11-20 ワイス 卵胞刺激ホルモン受容体（ｆｓｈ−ｒ）アンタゴニストとしてのピロロベンゾジアゼピンおよびヘテロ環状カルボキサミド誘導体
JP2008540564A (ja) * 2005-05-12 2008-11-20 ワイス 卵胞刺激ホルモン受容体（ｆｓｈ−ｒ）アンタゴニストとしてのピロロベンゾジアゼピン、ヘテロアリール、アリールおよびシクロアルキルアミノケトン誘導体
JP2008543765A (ja) 2005-06-09 2008-12-04 ワイス 卵胞刺激ホルモンレセプターアンタゴニストとしてのピロロベンゾジアゼピンピリジンカルボキサミドおよび誘導体
US20100061976A1 (en) * 2008-07-24 2010-03-11 Searete Llc, A Limited Liability Corporation Of The State Of Delaware Method for treating or preventing osteoporosis by reducing follicle stimulating hormone to cyclic physiological levels in a mammalian subject
RU2720237C2 (ru) 2013-11-18 2020-04-28 Форма Терапеутикс, Инк. Композиции, содержащие бензопиперазин, в качестве ингибиторов бромодоменов вет
HRP20210431T1 (hr) * 2013-11-18 2021-05-14 Forma Therapeutics, Inc. Pripravci tetrahidrokinolina kao inhibitori bet bromodomene
WO2019055869A1 (fr) 2017-09-15 2019-03-21 Forma Therapeutics, Inc. Compositions de tétrahydroimidazo quinoléine utilisées en tant qu'inhibiteurs de cbp/p300
CN112513038B (zh) 2018-06-29 2023-01-10 福马疗法公司 抑制creb结合蛋白(cbp)
AR118362A1 (es) 2019-03-15 2021-09-29 Forma Therapeutics Inc Inhibición de la proteína de unión al elemento de respuesta a amp cíclico (creb)
US11795168B2 (en) 2020-09-23 2023-10-24 Forma Therapeutics, Inc. Inhibiting cyclic amp-responsive element-binding protein (CREB) binding protein (CBP)
US11801243B2 (en) 2020-09-23 2023-10-31 Forma Therapeutics, Inc. Bromodomain inhibitors for androgen receptor-driven cancers

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Publication number Priority date Publication date Assignee Title
WO2000008015A2 (fr) * 1998-08-07 2000-02-17 Applied Research Systems Ars Holding N.V. Analogues de l'hormone de stimulation des follicules pour traiter l'infertilite
US6200963B1 (en) * 1999-03-31 2001-03-13 American Home Products Corporation Aryl sulfonic acids as FSH antagonists

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US2686182A (en) * 1950-12-07 1954-08-10 Basf Ag O-hydroxy-dihydro-quinoline carboxylic acids
ATE86484T1 (de) 1987-08-08 1993-03-15 Akzo Nv Kontrazeptives implantat.
SK280617B6 (sk) * 1992-01-16 2000-05-16 Hoechst Aktiengesellschaft Arylcykloalkylové deriváty, spôsob ich prípravy, f
EP1041066A1 (fr) * 1994-12-22 2000-10-04 Ligand Pharmaceuticals Incorporated Composés modulateurs des récepteurs de stéroides et procédés d'utilisation
IL159288A0 (en) * 2001-07-02 2004-06-01 Akzo Nobel Nv Tetrahydroquinoline derivatives
TWI306855B (en) * 2002-12-20 2009-03-01 Organon Nv Tetrahydroquinoline derivatives

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000008015A2 (fr) * 1998-08-07 2000-02-17 Applied Research Systems Ars Holding N.V. Analogues de l'hormone de stimulation des follicules pour traiter l'infertilite
US6200963B1 (en) * 1999-03-31 2001-03-13 American Home Products Corporation Aryl sulfonic acids as FSH antagonists

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9174940B2 (en) 2007-08-31 2015-11-03 Merck Sharp & Dohme B.V. TSH receptor antagonizing tetrahydroquinoline compounds

Also Published As

Publication number Publication date
JP2006512346A (ja) 2006-04-13
AU2003303221B2 (en) 2009-09-17
SI1578727T1 (sl) 2008-08-31
CA2508923C (fr) 2011-09-20
RU2328487C2 (ru) 2008-07-10
MXPA05006772A (es) 2005-09-08
AR042629A1 (es) 2005-06-29
CL43546B (es) 2005-04-08
RS20050458A (sr) 2007-08-03
ES2304544T3 (es) 2008-10-16
RU2005122924A (ru) 2006-01-27
WO2004056779A2 (fr) 2004-07-08
RS51196B (sr) 2010-12-31
DE60320457D1 (de) 2008-05-29
TWI322012B (en) 2010-03-21
BR0317514A (pt) 2005-11-16
PL376997A1 (pl) 2006-01-23
US7674909B2 (en) 2010-03-09
PE20040799A1 (es) 2004-12-02
NZ540577A (en) 2006-12-22
AU2003303221A1 (en) 2004-07-14
CA2508923A1 (fr) 2004-07-08
UA80303C2 (en) 2007-09-10
JP4545000B2 (ja) 2010-09-15
EP1578727B1 (fr) 2008-04-16
TW200418471A (en) 2004-10-01
EP1578727A2 (fr) 2005-09-28
DE60320457T2 (de) 2009-06-04
PT1578727E (pt) 2008-05-23
DK1578727T3 (da) 2008-08-04
ATE392416T1 (de) 2008-05-15
US20060167047A1 (en) 2006-07-27

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